Inhibitory effect of a redox-silent analogue of tocotrienol on hypoxia adaptation in prostate cancer cells

Anticancer Drugs. 2017 Mar;28(3):289-297. doi: 10.1097/CAD.0000000000000460.

Abstract

Prostate cancer (PCa) is one of the most common cancers in Western countries and acquires a malignant phenotype, androgen-independent growth. PCa under hypoxia often has resistance to chemotherapy and radiotherapy. However, an effective therapy against PCa under hypoxia has not yet been established. In this report, we investigated the inhibitory effect of a redox-silent analogue of tocotrienol on the survival of a human androgen-independent PCa cell line (PC3) under hypoxia. We found that the redox-silent analogue exerted a cytotoxic effect on PC3 cells in a dose-dependent manner irrespective of either hypoxia or normoxia. Moreover, under hypoxia, the analogue dose dependently reduced the protein levels of hypoxia-inducible factor (HIF)-1α and HIF-2α. In addition, a specific inhibitor toward HIF-1α induced cytotoxicity on PC3 cells, whereas selective inhibition of HIF-2α exerted no effect. Furthermore, suppression of HIFs levels by the analogue in hypoxic PC3 cells was closely associated with the inactivation of Fyn, a member of the nonreceptor tyrosine kinase family, as confirmed by the action of a specific inhibitor toward the kinase (PP2). Taken together, these results suggest that the tocotrienol analogue could inhibit the survival of PC3 cells under hypoxia, mainly by the inhibition of Fyn/HIF-1α signaling, and this may lead to the establishment of a new effective therapy for androgen-independent PCa.

MeSH terms

  • Adaptation, Physiological / drug effects
  • Antineoplastic Agents / pharmacology
  • Basic Helix-Loop-Helix Transcription Factors / antagonists & inhibitors
  • Basic Helix-Loop-Helix Transcription Factors / metabolism
  • Cell Hypoxia / drug effects*
  • Cell Hypoxia / physiology
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism
  • Male
  • Oxidation-Reduction
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism*
  • Prostatic Neoplasms, Castration-Resistant / drug therapy*
  • Prostatic Neoplasms, Castration-Resistant / metabolism*
  • Proto-Oncogene Proteins c-fyn / antagonists & inhibitors
  • Proto-Oncogene Proteins c-fyn / metabolism
  • Tocotrienols / pharmacology*

Substances

  • 6-O-carboxypropyl-alpha-tocotrienol
  • Antineoplastic Agents
  • Basic Helix-Loop-Helix Transcription Factors
  • HIF1A protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Tocotrienols
  • endothelial PAS domain-containing protein 1
  • FYN protein, human
  • Proto-Oncogene Proteins c-fyn